Shi K, Li C, He B
Department of Chemistry, Nankai University, Tianjin.
Sheng Wu Yi Xue Gong Cheng Xue Za Zhi. 2000 Mar;17(1):21-4.
A novel magnetic drug carrier-carboxymethyl dextran magnetic nanoparticles(CMD MNPs) was prepared. Adriamycin (ADR) was coupled with two types of carrier-neutral dextran MNPs and anionic CMD MNPs, by periodate oxidation. The physico-chemical characteristics and the magnetic guidance effects in vitro and in vivo of ADR-CMD MNPs were studied. The distribution profiles of liver and spleen in mice were studied for both ADR-dextran conjugate MNPs and ADR-CMD conjugate MNPs. The results showed ADR-CMD conjugate MNPs possessed superparamagnetism, the mean diameter was 56 nm, the mass magnetic susceptibility was 1.06 x 10(-4) emu.g-1, and the drug loading was 12.4%. The distribution profiles in liver and spleen revealed that conjugation with neutral dextran MNPs, excessive accumulation of loaded ADR was found in liver and spleen after intravenous administration, while conjugation with CMD MNPs gave a markedly lower concentration in these organs, which indicated less uptake of ADR-CMD conjugate MNPs by reticuloendothelial system(RES) and the advantage of delivering loaded drug to sites other than the RES; thus it opens a new perspective for the active delivery of drug.
制备了一种新型磁性药物载体——羧甲基葡聚糖磁性纳米颗粒(CMD MNPs)。通过高碘酸盐氧化法,将阿霉素(ADR)与两种类型的载体——中性葡聚糖磁性纳米颗粒和阴离子型CMD MNPs偶联。研究了ADR-CMD MNPs的理化特性以及其在体外和体内的磁导向作用。对ADR-葡聚糖共轭磁性纳米颗粒和ADR-CMD共轭磁性纳米颗粒在小鼠体内肝脏和脾脏的分布情况进行了研究。结果表明,ADR-CMD共轭磁性纳米颗粒具有超顺磁性,平均直径为56 nm,质量磁化率为1.06×10(-4) emu·g-1,载药量为12.4%。肝脏和脾脏的分布情况显示,与中性葡聚糖磁性纳米颗粒偶联后,静脉注射后肝脏和脾脏中发现负载的ADR过度蓄积,而与CMD MNPs偶联后,这些器官中的浓度明显较低,这表明ADR-CMD共轭磁性纳米颗粒被网状内皮系统(RES)摄取较少,以及将负载药物输送到RES以外部位的优势;因此,它为药物的主动递送开辟了新的前景。